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Giang Le, Nick Vandegraaff, David I Rhodes, Eric D Jones, Jonathan A V Coates, Long Lu, Xinming Li, Changjiang Yu, Xiao Feng, John J Deadman
A series of novel HIV integrase inhibitors active against rategravir resistant strains are reported. Initial SAR studies revealed that activities against wild-type virus were successfully maintained at single digit nanomolar level with a wide range of substitutions. However, inclusion of nitrogen-based cyclic substitutions was crucial for achieving potency against mutant viruses. Several compounds with excellent activities against wild-type virus as well as against the viruses with the mutations Q148H/G140S or N155H/E92Q were reported...
September 1, 2010: Bioorganic & Medicinal Chemistry Letters
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